DCA-VPA Combination Modulates Gene Expression for Infection Treatment

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Solution Overview

Problem

Current treatments for viral and bacterial infections, as well as inflammatory diseases, often fail to effectively manage inflammation and immune response, leading to prolonged recovery times and potential organ damage.

Innovation Solution

The use of a combination of sodium dichloroacetate (DCA) and valproic acid (VPA) salts, which inhibit inflammatory reactions, modulate the immune response, and promote anti-inflammatory biological pathways, thereby reducing the severity of infections and inflammation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for viral and bacterial infections, then the standard therapy is administered, but inflammation and immune response are not effectively managed, leading to prolonged recovery times and potential organ damage

Engineering Contradiction:
Improveeffectiveness of inflammation managementVSAvoidrecovery time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent combines two existing drugs with different mechanisms of action - dichloroacetate (which suppresses glycolysis and lactic acid production) and valproic acid (which has immunomodulating effects). This combination creates a synergistic effect that more effectively manages inflammation and immune response than either drug alone, thereby improving reliability of treatment and reducing recovery time

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If dichloroacetate is administered to suppress glycolysis and lactic acid production, then metabolic acidosis is reduced, but the transport of DCA into cells is limited without activation

Engineering Contradiction:
Improvesuppression of metabolic acidosisVSAvoidintracellular transport efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

Valproic acid acts as an intermediary that activates the SLC5A8 transporter, which is responsible for transporting dichloroacetate into cells. By demethylating the SLC5A8 gene promoter, VPA increases transporter expression and activity, thereby enhancing the intracellular delivery of DCA and improving its metabolic effects

Inventive Principle:
Principle #24Intermediary (Mediator)

3Productivity

If valproic acid is used to activate SLC5A8 transporter, then intracellular DCA transport is enhanced, but the mechanism requires demethylation processes

Engineering Contradiction:
ImproveDCA transport into cellsVSAvoidmechanism complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

Valproic acid changes the epigenetic parameters of the SLC5A8 gene by removing methyl groups from the promoter region through demethylation mechanisms. This parameter change increases the expression level of the SLC5A8 transporter, thereby enhancing DCA transport into cells without requiring complex external delivery systems

Inventive Principle:
Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The DCA-VPA combination demonstrates a synergistic anti-inflammatory effect by enhancing the transport of DCA into cells, reducing lactic acid production, and modulating gene expression related to inflammation and immune response, leading to improved treatment outcomes for various infections and inflammatory diseases.

Implementation Method 1

VPA activates intracellular expression of the SLC5A8 gene by demethylation mechanisms, which enhances the transport of DCA into the mitochondria of the cell

Methodology Applied
Scientific EffectDemethylation:

Implementation Method 2

The component of the combination sodium dichloroacetate (DCA) suppresses glycolysis and the development of metabolic acidosis. By suppressing the production of lactic acid

Methodology Applied
Scientific EffectGlycolysis suppression:

Implementation Method 3

By suppressing the production of lactic acid, DCA also inhibits the release of pro-inflammatory cytokines

Methodology Applied
Scientific EffectAnti-inflammatory effect:

Implementation Method 4

Valproic acid (VPA) has an immunomodulating effect that suppresses inflammatory reactions caused by viruses or bacteria

Methodology Applied
Scientific EffectImmunomodulation:

Data Source

PatentEP4512393A1Combination of sodium dichloroacetate and valproic acid salts for the treatment of viral and bacterial infections and inflammatory diseases
Publication Date: 2025.02.26 LIETUVOS SVEIKATOS MOKSLU UNIVS
  • EP4512393A1 patent drawingFigure 1~2
  • EP4512393A1 patent drawingFigure 3~4
  • EP4512393A1 patent drawingFigure 5~6

AI summary

The invention provides preclinical in vivo and in vitro and clinical trials in vitro data as well as the expression of genes related to the inflammation and immune response to the medicinal product under development, using differential gene expression analysis of sequencing data. The evaluation of the effect of the new DCA-VPA combination based on research data leads to the conclusion that treatment with the DCA-VPA combination under development influences gene regulation disorders caused by viral and bacterial infection in the body and is suitable for correcting or inhibiting pathological processes at the molecular level. Based on the results obtained from this advanced technology, a new medicinal product consisting of a combination of dichloroacetate and valproic acid medicinal products is being developed for the treatment of viral and bacterial infections and inflammatory diseases, which can improve the course of the treated disease, accelerate patient recovery, survival, quality of life and reduce healthcare costs.